1630086-20-2
中文名称
KIRA8 (AMG-18)
英文名称
Amgen IRE1α Inhibitor
CAS
1630086-20-2
分子式
C31H29ClN6O3S
分子量
601.12
MOL 文件
1630086-20-2.mol
更新日期
2024/06/06 11:49:20
1630086-20-2 结构式
基本信息
中文别名
化合物KIRA8(S)-2-氯-N-(6-甲基-5-((3-(2-(哌啶-3-基氨基)嘧啶-4-基)吡啶-2-基)氧基)萘-1-基)苯磺酰胺
英文别名
Kira8KIRA8 (AMG-18)
IRE-1 INHIBITOR
Amgen IRE1α Inhibitor
Benzenesulfonamide, 2-chloro-N-[6-methyl-5-[[3-[2-[(3S)-3-piperidinylamino]-4-pyrimidinyl]-2-pyridinyl]oxy]-1-naphthalenyl]-
物理化学性质
沸点812.6±75.0 °C(Predicted)
密度1.383±0.06 g/cm3(Predicted)
储存条件-20°C储存
溶解度Water:30.0(Max Conc. mg/mL);49.91(Max Conc. mM)
酸度系数(pKa)7.66±0.30(Predicted)
形态Solid
颜色Light yellow to yellow
常见问题列表
生物活性
Kira8 (AMG-18) 是一种单选择性 IRE1α 抑制剂，可以变构减弱 IRE1α RNase 活性，IC50 为 5.9 nM。靶点
IRE1α
IC50: 5.9 nM (IRE1α RNase)
体外研究
Kira8 blocks IRE1α oligomerization, and potently inhibits IRE1α RNase activity against XBP1 and Ins2 RNAs. Kira8 more potently reduces IRE1α-driven apoptosis in INS-1 cells than KIRA6 and also reverses XBP1 splicing promoted by GNF-2.
体内研究
Male
Ins2
+/Akita
mice are injected i.p. with KIRA8 (50 mg/kg; daily; for 35 days), significant reduction of hyperglycemia become apparent over several weeks.
One week treatment of pre-diabetic NODs mice with Kira8 (50 mg/kg; i.p.; once a day) leads to significant reductions in islet XBP1 splicing and TXNIP mRNAs, and preserves Ins1/Ins2, BiP and MANF mRNAs.
| Animal Model: | Male Ins2 +/Akita mice |
| Dosage: | 50 mg/kg |
| Administration: | Injected i.p.; daily; for 35 days |
| Result: | Significant reduction of hyperglycemia became apparent over several weeks. |